The term “anti-inflammatory” refers to the property of a compound that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation.
Nonsteroidal anti-inflammatory drugs (NSAIDs) are a class of drugs that provide analgesic and antipyretic (fever-reducing) effects, and, in higher doses, anti-inflammatory effects. The term “nonsteroidal” distinguishes these drugs from steroids, which, among a broad range of other effects, have a similar eicosanoid-depressing, anti-inflammatory action. As analgesics, NSAIDs are unusual in that they are non-narcotic. The most prominent members of the NSAID group of drugs are aspirin, ibuprofen and naproxen.
The widespread use of NSAIDs has meant that the adverse effects of these drugs are well known and have become increasingly prevalent as the population ages. The two main adverse drug reactions (ADRs) associated with NSAID use are gastrointestinal (GI) and renal effects. These effects are dose-dependent and, in many cases, severe enough to pose the risk of ulcer perforation, upper gastrointestinal bleeding, and death, thereby limiting the use of NSAID therapy. An estimated 10-20% of NSAID patients experience dyspepsia, and NSAID-associated upper GI adverse events are estimated to result in 103,000 hospitalizations and 16,500 deaths per year in the United States and represent 43% of drug-related emergency visits. Thus, the clinical problems with NSAIDs and the need for replacement anti-inflammatories are well recognized.
For at least these reasons, it would be desirable to find substitutes for the current NSAIDs having increased anti-inflammatory potency and a higher safety margin.